Stephen Walter O'Connor

US Patent:

20020193596, Dec 19, 2002

Filed:

Oct 30, 2001

Appl. No.:

09/984411

Inventors:

Said Sebti - Tampa FL, US
Andrew Hamilton - Guilford CT, US
David Augeri - Kenosha WI, US
Kenneth Barr - Chicago IL, US
Greg Donner - Mundelein IL, US
Stephen Fakhoury - Mundelein IL, US
Stephen O'Connor - Wilmette IL, US
Saul Rosenberg - Grayslake IL, US
Wang Shen - Gurnee IL, US
Bruce Szczepankiewicz - Lindenhurst IL, US
Indrani Gunawardana - Libertyville IL, US

Assignee:

University of Pittsburgh - Pittsburgh PA

International Classification:

C 07D 4 5/02
C07D307/56

US Classification:

544/238000, 549/321000, 548/252000, 544/333000, 544/405000

Abstract:

Compounds having the formula or a pharmaceutically acceptable salt thereof wherein Ris (a) hydrogen, (b) loweralkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halo, (g) haloalkyl, (h) aryl-L—, and (i) heterocyclic-L—; Ris selected from (a) (b) —C(O)NH—CH(R)—C(O)OR, (c) (d) —C(O)NH—CH(R)—C(O)NHSOR(e) —C(O)NH—CH(R)-tetrazolyl, (f) —C(O)NH-heterocyclic, and (g) —C(O)NH—CH(R)—C(O)NRR; Ris heterocyclic, aryl, substituted or unsubstituted cycloalkyl; Ris hydrogen, lower alkyl, haloalkyl, halogen, aryl, arylakyl, heterocyclic, or (heterocyclic)alkyl; Lis absent or is selected from (a) —L—N(R)—L—, (b) —L—O—L—, (c) —L—S(O)—L— (d) —L-L—C(W)—N(R)—L—, (e) —L-L—S(O)—N(R)—L—, (f) —L—N(R)—C(W)—L-L—, (g) —L—N(R)—S(O)—L—L—, (h) optionally substituted alkylene, (i) optionally substituted alkenylene, and (j) optionally substituted alkynylene are inhibitors of protein isoprenyl transferases. Also disclosed are protein isoprenyl transferase inhibiting compositions and a method of inhibiting protein isoprenyl transferases.

US Patent:

62042939, Mar 20, 2001

Filed:

May 7, 1998

Appl. No.:

9/073807

Inventors:

Said M. Sebti - Tampa FL
Andrew D. Hamilton - Guilford CT
David J. Augeri - Kenosha WI
Kenneth J. Barr - Chicago IL
Stephen A. Fakhoury - Mundelein IL
David A. Janowick - Beach Park IL
Douglas M. Kalvin - Buffalo Grove IL
Stephen J. O'Connor - Wilmette IL
Saul H. Rosenberg - Grayslake IL
Wang Shen - Gurnee IL
Rolf E. Swenson - Grayslake IL
Bryan K. Sorensen - Waukegan IL
Gerard M. Sullivan - Round Lake Beach IL
Andrew S. Tasker - Simi Valley CA
James T. Wasicak - Waterford WI
Lissa T. J. Nelson - Highland Park IL
Kenneth J. Henry - Fishers IN
Le Wang - Mundelein IL
Gang Liu - Gurnee IL
Indrani W. Gunawardana - Libertyville IL

Assignee:

University of Pittsburgh - Pittsburgh PA

International Classification:

C07C26302
C07C30300
A61K 3138

US Classification:

514570

Abstract:

Compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R. sub. 1 is (a) hydrogen, (b) loweralkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halo, (g) haloalkyl, (h) aryl-L. sub. 2 --, and (i) heterocyclic-L. sub. 2 --; R. sub. 2 is selected from ##STR2## (b) --C(O)NH--CH(R. sub. 14)--C(O)OR. sub. 15, ##STR3## (d) --C(O)NH--CH(R. sub. 14)--C(O)NHSO. sub. 2 R. sub. 16, (e) --C(O)NH--CH(R. sub. 14)-tetrazolyl, (f) --C(O)NH-heterocyclic, and (g) --C(O)NH--CH(R. sub. 14)--C(O)NR. sub. 17 R. sub. 18 ; R. sub. 3 is heterocyclic, aryl, substituted or unsubstituted cycloalkyl; R. sub. 4 is hydrogen, lower alkyl, haloalkyl, halogen, aryl, arylakyl, heterocyclic, or (heterocyclic)alkyl; L. sub. 1 is absent or is selected from (a) --L. sub. 4 --N(R. sub. 5)--L. sub. 5 --, (b) --L. sub. 4 --O--L. sub.

US Patent:

62218654, Apr 24, 2001

Filed:

May 7, 1998

Appl. No.:

9/073795

Inventors:

Said M. Sebti - Tampa FL
Andrew D. Hamilton - Guilford CT
Kenneth J. Barr - Chicago IL
Stephen A. Fakhoury - Mundelein IL
Stephen J. O'Connor - Wilmette IL
Saul H. Rosenberg - Grayslake IL
Wang Shen - Gurnee IL
Bryan K. Sorensen - Waukegan IL
Gerard M. Sullivan - Round Lake Beach IL
James T. Wasicak - Waterford IL
Kenneth J. Henry - Fishers IN
Le Wang - Mundelein IL

Assignee:

University of Pittsburgh - Pittsburgh PA

International Classification:

A61K 315377
A61K 314025
C07D40106
C07D41306
C07D20706

US Classification:

5142355

Abstract:

Compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R. sub. 1 is (a) hydrogen, (b) loweralkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halo, (g) haloalkyl, (h) aryl-L. sub. 2 --, and (i) heterocyclic-L. sub. 2 --; R. sub. 2 is selected from (a) ##STR2## (b) --C(O)NH--CH(R. sub. 14)--C(O)OR. sub. 15, ##STR3## (d) --C(O)NH--CH(R. sub. 14)--C(O)NHSO. sub. 2 R. sub. 16, (e) --C(O)NH--CH(R. sub. 14)-tetrazolyl, (f) --C(O)NH-heterocyclic, and (g) --C(O)NH--CH(R. sub. 14)--C(O)NR. sub. 17 R. sub. 18 ; R. sub. 3 is substituted or unsubstituted heterocyclic or aryl, substituted or unsubstituted cycloalkyl or cycloalkenyl, ##STR4## and --P(W)R. sup. R3 R. sup. R3 '; R. sub. 4 is hydrogen, lower alkyl, haloalkyl, halogen, aryl, arylakyl, heterocyclic, or (heterocyclic)alkyl; L. sub. 1 is absent or is selected from (a) --L. sub. 4 --N(R. sub. 5)--L. sub.

US Patent:

63100959, Oct 30, 2001

Filed:

May 7, 1998

Appl. No.:

9/073794

Inventors:

Said M. Sebti - Tampa FL
Andrew D. Hamilton - Guilford CT
David J. Augeri - Kenosha WI
Kenneth J. Barr - Chicago IL
Stephen A. Fakhoury - Mundelein IL
David A. Janowick - Beach Park IL
Douglas M. Kalvin - Buffalo Grove IL
Stephen J. O'Connor - Wilmette IL
Saul H. Rosenberg - Grayslake IL
Wang Shen - Gurnee IL
Rolf E. Swenson - Grayslake IL
Bryan K. Sorenson - Waukegan IL
Gerard M. Sullivan - Round Lake Beach IL
Andrew S. Tasker - Simi Valley CA
James T. Wasicak - Waterford WI
Lissa T. J. Nelson - Highland Park IL
Kenneth J. Henry - Fishers IN
Le Wang - Mundelein IL

Assignee:

University of Pittsburgh - Pittsburgh PA

International Classification:

A61K 31192
C07C 53134

US Classification:

514539

Abstract:

Compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R. sub. 1 is (a) hydrogen, (b) loweralkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halo, (g) haloalkyl, (h) aryl-L. sub. 2 --, and (i) heterocyclic-L. sub. 2 --; R. sub. 2 is selected from (a) ##STR2## (b) --C(O)NH--CH(R. sub. 14)--C(O)OR. sub. 15, ##STR3## (d) --C(O)NH--CH(R. sub. 14)--C(O)NHSO. sub. 2 R. sub. 16, (e) --C(O)NH--CH(R. sub. 14)-tetrazolyl, (f) --C(O)NH-heterocyclic, and (g) --C(O)NH--CH(R. sub. 14)--C(O)NR. sub. 17 R. sub. 18 ; R. sub. 3 is substituted or unsubstituted heterocyclic or aryl, substituted or unsubstituted cycloalkyl or cycloalkenyl, ##STR4## and --P(W)R. sup. R3 R. sup. R3' ; R. sub. 4 is hydrogen, lower alkyl, haloalkyl, halogen, aryl, arylakyl, heterocyclic, or (heterocyclic)alkyl; L. sub. 1 is absent or is selected from (a) --L. sub. 4 --N(R. sub. 5)--L. sub.